Document Report Card

ID: ALA1135522

Journal: J Med Chem

Title: Novel retinoid X receptor antagonists: specific inhibition of retinoid synergism in RXR-RAR heterodimer actions.

Authors: Takahashi B, Ohta K, Kawachi E, Fukasawa H, Hashimoto Y, Kagechika H.

Abstract: Several 2-(arylamino)pyrimidine-5-carboxylic acids were designed as novel retinoid X receptor (RXR) antagonists. Compound 6a or 6b alone did not exhibit differentiation-inducing activity toward HL-60 cells and did not affect the activity of a retinoic acid receptor (RAR) agonist, Am80, but did inhibit the synergistic activity of an RXR agonist, PA024 (3), in the presence of Am80. The activity of 6 was ascribed to selective antagonism at the RXR site of RXR-RAR heterodimers.

CiteXplore: 12139443

DOI: 10.1021/jm0255320